Crystalline 2-(3,5-Bis(trifluoromethyl)phenyl)-N-(4-(4-fluoro-2-methylphenyl)-6-((7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)pyridin-3-yl)-N,2-dimethyl-propanamide of the formula (I), their use in therapy, and process for the preparation of the same

Abstract

The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.

What is claimed is: 
     
       1. A compound of formula (I): 
       
         
           
           
               
               
           
         
         in a crystalline anhydrate form and having an X-ray powder diffraction pattern comprising 2 theta angle peaks at 7.9°±0.1, 9.8°±0.1, and 10.8°±0.1 which correspond respectively to d-spacing at 11.1, 9.0, and 8.2 Å. 
       
     
     
       2. The compound according to  claim 1 , having substantially the same X-ray powder diffraction pattern as in  FIG. 1 . 
     
     
       3. The compound according to  claim 1 , having an X-ray powder diffraction pattern comprising 2 theta angle peaks at the following positions: 4.3°±0.1, 7.9°±0.1, 9.8°±0.1, 10.7°±0.1, 10.8°±0.1, 13.3°±0.1, 14.0°±0.1, 15.1±0.1° degrees, which correspond respectively to d-spacing at 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3 and 5.9 Å. 
     
     
       4. The compound according to  claim 1 , having an X-ray powder diffraction pattern comprising 2 theta angle peaks at the following positions: 4.3°±0.1, 7.9°±0.1, 9.8°±0.1, 10.7°±0.1, 10.8°±0.1, 13.1°±0.1, 13.2°±0.1, 13.3°±0.1, 14.0°±0.1, 14.4°±0.1, 15.0°±0.1, 15.1°±0.1, 15.7°±0.1, 15.9°±0.1, 16.3°±0.1, 16.5°±0.1, 16.8°±0.1, 17.0°±0.1, 17.4°±0.1, 17.5°±0.1, 18.1°±0.1, 18.2°±0.1, 18.7°±0.1, 19.4°±0.1, 19.7°±0.1, 20.0°±0.1, 20.1°±0.1, 20.2°±0.1, 20.5°±0.1, 20.7°±0.1, 21.5°±0.1, and 21.8±0.1° degrees, which correspond respectively to d-spacings at 20.4, 11.1, 9.0, 8.3, 8.2, 6.8, 6.7, 6.6, 6.3, 6.1, 5.9, 5.9, 5.6, 5.6, 5.4, 5.4, 5.3, 5.2, 5.1, 5.1, 4.9, 4.9, 4.7, 4.6, 4.5, 4.4, 4.4, 4.4, 4.3, 4.3, 4.1 and 4.1 Å. 
     
     
       5. The compound according to  claim 1 , having a  13 C solid state nuclear magnetic resonance spectrum comprising chemical shifts at 175.03±0.2, 163.30±0.2, 158.66±0.2, 156.50±0.2, 149.79±0.2, 148.17±0.2, 146.96±0.2, 139.56±0.2, 133.19±0.2, 132.32±0.2, 129.76±0.2, 126.5±0.2, 124.15±0.2, 120.37±0.2, 119.20±0.2, 118.16±0.2, 112.83±0.2, 70.62±0.2, 67.61±0.2, 64.96±0.2, 59.89±0.2, 57.08±0.2, 55.50±0.2, 52.41±0.2, 48.35±0.2, 40.79±0.2, 32.75 and 21.12±0.2 ppm. 
     
     
       6. A pharmaceutical composition comprising the compound according to  claim 1  and a pharmaceutically acceptable carrier and/or diluent. 
     
     
       7. A pharmaceutical composition according to  claim 6  further comprising one or more additional pharmaceutically acceptable carriers or diluents. 
     
     
       8. A method for the treatment or prophylaxis of psychotic disorders, depression, mood disorders, anxiety, sleep disorders and alcohol dependence comprising administering to the mammal, an effective amount of the compound according to  claim 1 . 
     
     
       9. A compound of formula (I): 
       
         
           
           
               
               
           
         
         in crystalline anhydrate form, having the same  13 C solid state nuclear magnetic resonance spectrum as in  FIG. 3 .